nilotinib (Rx)

Brand and Other Names:Tasigna
  • Print

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 150mg
  • 200mg

Chronic Myeloid Leukemia

Newly diagnosed Ph+ CML-CP

  • Indicated for initial treatment of newly diagnosed Philadelphia chromosome positive (Ph+) chronic phase (CP) chronic myeloid leukemia (CML)
  • 300 mg PO q12hr

Resistant or intolerant

  • Indicated for treatment of CP and accelerated phase (AP) Ph+ CML in patients resistant to or intolerant to prior therapy that included imatinib
  • 400 mg PO q12hr

Gastrointestinal Stromal Tumors (Orphan)

Orphan indication sponsor

  • Novartis Pharmaceuticals Corporation; One Health Plaza; East Hanover, NJ 07936-1080

Dosage Modifications

Neutropenia and thrombocytopenia

  • Adults with newly diagnosed Ph+ CP-CML or resistant or intolerant CP and AP Ph+ CML
    • Absolute neutrophil count (ANC) <1 x 10^9/L or platelet <50x 10^9/L: Stop nilotinib and monitor blood counts
    • Within 2 weeks of recovery: Resume original dose if ANC >1 x 10^9/L & platelet >50 x 10^9/L
    • If levels remain low for >2 weeks: Reduce dose to 400 mg qDay

QT Prolongation (QTc >480 msec)

  • Withhold drug and analyze serum potassium and magnesium; if below lower limit of normal, correct with supplements to within normal limits
  • Review concomitant medications for additive effects or interactions that increase nilotinib systemic exposure
  • Resume within 2 weeks at prior dose if QTc returns to <450 msec and to within 20 msec of baseline
  • If QTc is between 450-480 msec after 2 weeks, reduce nilotinib dose to 400 mg qDay
  • Discontinue if QTc returns to >480 msec despite reducing the dose to 400 mg/day
  • Repeat ECG ~7 days after any dose adjustment

Moderate or severe nonhematologic toxicity

  • Resume treatment at 400 mg qDay if previous dose was 300 mg qDay (newly diagnosed Ph+ CML-CP) or 400 mg BID (resistant or intolerant Ph+ CML-CP and CML-AP); discontinue treatment if prior dose was 400 mg qDay
  • If clinically appropriate, consider re-escalate dose to 300 mg qDay (newly diagnosed Ph+ CML-CP) or 400 mg BID (resistant or intolerant Ph+ CML-CP and CML-AP)

Elevated serum lipase or amylase ≥Grade 3

  • Withhold nilotinib, and monitor serum lipase or amylase
  • Resume treatment at 400 mg qDay if serum lipase or amylase returns to ≤Grade 1

Elevated bilirubin or alanine transaminase (ALT)/aspartate transaminase (AST) ≥Grade 3

  • Withhold nilotinib, monitor bilirubin
  • Resume treatment at 400 mg qDay if serum bilirubin returns to ≤Grade 1

Hepatic impairment

  • Newly diagnosed Ph+ CML (chronic phase at 300 mg BID)
    • Mild, moderate, or severe hepatic (Child-Pugh A to C): Start initial dose at 200 mg BID; if tolerated, may increase to 300 mg BID
  • Resistant or intolerant Ph+ CML (chronic phase or accelerated phase at 400 mg BID)
    • Mild or moderate (Child-Pugh A to B): Start initial dose at 300 mg BID; if tolerated, may increase to 400 mg BID
    • Severe (Child-Pugh C): Start initial dose at 200 mg BID; if tolerated, may increase to 300 mg BID, and then 400 mg BID

Renal impairment

  • Clinical studies have not been performed in patients with impaired renal function
  • Since nilotinib and its metabolites are not renally excreted, a decrease in total body clearance is not anticipated in patients with renal impairment

Consider discontinuation of treatment after a sustained molecular response

  • Monitor BCR-ABL transcript levels and complete blood count (CBC) with differential in patients who have discontinued therapy monthly for 1 year, then q6Weeks for the second year, and q12Weeks thereafter
  • Newly diagnosed Ph+ CML-CP
    • Treatment with nilotinib for at least 3 years
    • Maintain a molecular response of at least MR4.0 (corresponding to = BCR-ABL/ABL ≤0.01% IS) for 1 year prior to discontinuation of therapy
    • Achieved an MR4.5 for the last assessment taken immediately prior to discontinuation of therapy
    • Been confirmed to express the typical BCR-ABL transcripts (e13a2/b2a2 or e14a2/b3a2)
    • No history of accelerated phase or blast crisis
    • No history of prior attempts of treatment-free remission discontinuation that resulted in relapse
  • Patients with Ph+ CML-CP that are resistant or intolerant to treatment with imatinib
    • Treatment with nilotinib for at least 3 years
    • Previously treated with imatinib only prior to treatment with nilotinib
    • Achieved a molecular response of MR.4.5 (corresponding to = BCR-ABL/ABL ≤0.0032% IS)
    • Sustained an MR4.5 for a minimum of one year immediately prior to discontinuation of therapy
    • Been confirmed to express the typical BCR-ABL transcripts (e13a2/b2a2 or e14a2/b3a2)
    • No history of accelerated phase or blast crisis
    • No history of prior attempts of treatment-free remission discontinuation that resulted in relapse

Reinitiating treatment if molecular response lost after discontinuing therapy

  • Newly diagnosed patients
    • Patients who lose MMR must reinitiate treatment within 4 weeks at the dose level prior to discontinuing treatment
    • Monitor BCR-ABL transcript levels monthly until major molecular response is re-established and q12Weeks thereafter
  • Resistant or intolerant Ph+ CML (chronic phase or accelerated phase)
    • Patients resistant or intolerant to prior treatment that included imatinib with confirmed loss of MR4.0 (2 consecutive measures separated by at least 4 weeks showing loss of MR4.0) or loss of MMR must reinitiate treatment within 4 weeks at the dose level prior to discontinuation of therapy
    • Monitor BCR-ABL transcript levels monthly until previous major molecular response or MR 4.0 is re-established and q12Weeks thereafter

Coadministration with strong CYP3A4 inhibitors

  • Avoid if possible; for patients who cannot avoid use of strong CYP3A4 inhibitors, monitor closely for QT prolongation
  • If patients must coadminister a strong CY3A4 inhibitor, reduce dose to 300 mg/day in patients with resistant or intolerant Ph+ CML or to 200 mg/day with newly diagnosed Ph+ CML-CP
  • However, there are no clinical data with this dose adjustment in patients receiving strong CYP3A4 inhibitors

Coadministration with strong CYP3A4 inducers

  • Avoid coadministration
  • Based on nonlinear pharmacokinetic profile of nilotinib, increasing the dose is unlikely to compensate for loss of nilotinib systemic exposure

Dosage Forms & Strengths

capsule

  • 50mg
  • 150mg
  • 200mg

Chronic Myeloid Leukemia

Indicated for initial treatment of newly diagnosed Philadelphia chromosome positive chronic phase chronic myeloid leukemia (Ph+ CP-CML) in children and adolescents aged ≥1 year

Also, indicated for children and adolescents aged ≥1 year with Ph+ CP-CML resistant or intolerant to prior tyrosine-kinase inhibitor (TKI) therapy

230 mg/m² PO BID, round to the nearest 50 mg dose; not to exceed 400 mg/dose

Continue treatment until disease progression or unacceptable toxicity occurs

Dosage Modifications

Neutropenia and thrombocytopenia

  • ANC <1 x 10^9/L and/or platelets <50x 10^9/L
    • Stop nilotinib and monitor blood counts
    • Resume within 2 weeks to original dose if ANC >1.5 x 109/L and/or platelets >75 x 109/L
    • If ANC remains low for >2 weeks: Reduce dose to 230 mg/m² qDay
    • If event occurs after dose reduction, consider discontinuing treatment

QT Prolongation (QTc >480 msec)

  • Withhold drug and analyze serum potassium and magnesium; if below lower limit of normal, correct with supplements to within normal limits
  • Review concomitant medications for additive effects or interactions that increase nilotinib systemic exposure
  • Resume within 2 weeks at prior dose if QTc returns to <450 msec and to within 20 msec of baseline
  • If QTc is between 450-480 msec after 2 weeks, reduce nilotinib dose to 230 mg/m² qDay
  • Discontinue if QTc returns to >480 msec despite dose reduction
  • Repeat ECG ~7 days after any dose adjustment

Moderate or severe non-hematologic toxicity

  • Interrupt nilotinib until toxicity has resolved
  • Resume treatment at 230 mg/m² qDay if previous dose was 230 mg/m² BID; discontinue treatment if prior dose was 230 mg/m² qDay
  • If clinically appropriate, consider re-escalation of the dose to 230 mg/m² BID

Elevated serum lipase or amylase ≥Grade 3

  • Interrupt nilotinib until the event returns to ≤Grade 1
  • Resume treatment at 230 mg/m² qDay if prior dose was 230 mg/m² BID; discontinue treatment if prior dose was 230 mg/m² qDay

Elevated bilirubin or AST/ALT ≥Grade 3

  • Interrupt nilotinib until the event returns to ≤Grade 1
  • Resume treatment at 230 mg/m² qDay if prior dose was 230 mg/m² BID; discontinue treatment if prior dose was 230 mg/m² qDay, and recovery to ≤Grade 1 takes >28 days

Consider discontinuation of treatment after a sustained molecular response

  • Monitor BCR-ABL transcript levels and complete blood count (CBC) with differential in patients who have discontinued therapy monthly for 1 year, then q6Weeks for the second year, and q12Weeks thereafter
  • Newly diagnosed Ph+ CML-CP
    • Treatment with nilotinib for at least 3 years
    • Maintain a molecular response of at least MR4.0 (corresponding to = BCR-ABL/ABL ≤0.01% IS) for 1 year prior to discontinuation of therapy
    • Achieved an MR4.5 for the last assessment taken immediately prior to discontinuation of therapy
    • Been confirmed to express the typical BCR-ABL transcripts (e13a2/b2a2 or e14a2/b3a2)
    • No history of accelerated phase or blast crisis
    • No history of prior attempts of treatment-free remission discontinuation that resulted in relapse
  • Patients with Ph+ CML-CP that are resistant or intolerant to treatment with imatinib
    • Treatment with nilotinib for at least 3 years
    • Previously treated with imatinib only prior to treatment with nilotinib
    • Achieved a molecular response of MR4.5 (corresponding to = BCR-ABL/ABL ≤ 0.0032% IS)
    • Sustained an MR4.5 for a minimum of 1 year immediately prior to discontinuation of therapy
    • Been confirmed to express the typical BCR-ABL transcripts (e13a2/b2a2 or e14a2/b3a2)
    • No history of accelerated phase or blast crisis
    • No history of prior attempts of treatment-free remission discontinuation that resulted in relapse

Reinitiation of treatment in patients who lose molecular response after discontinuation of therapy

  • Newly diagnosed patients
    • Patients who lose MMR must reinitiate treatment within 4 weeks at the dose level prior to discontinuing treatment
    • Monitor BCR-ABL transcript levels monthly until major molecular response is re-established and q12Weeks thereafter
  • Resistant or intolerant Ph+ CML (chronic phase or accelerated phase)
    • Patients resistant or intolerant to prior treatment that included imatinib with confirmed loss of MR4.0 (2 consecutive measures separated by at least 4 weeks showing loss of MR4.0) or loss of MMR must reinitiate treatment within 4 weeks at the dose level prior to discontinuation of therapy
    • Monitor BCR-ABL transcript levels monthly until previous major molecular response or MR 4.0 is re-established and q12Weeks thereafter

Coadministration with strong CYP3A4 inhibitors

  • Avoid if possible; for patients who cannot avoid use of strong CYP3A4 inhibitors, monitor closely for QT prolongation
  • However, there are no clinical data with this dose adjustment in patients receiving strong CYP3A4 inhibitors

Coadministration with strong CYP3A4 inducers

  • Avoid coadministration
  • Based on nonlinear pharmacokinetic profile of nilotinib, increasing the dose is unlikely to compensate for loss of nilotinib systemic exposure
Next:

Interactions

Interaction Checker

and nilotinib

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 

            Contraindicated (12)

            • arsenic trioxide

              arsenic trioxide and nilotinib both increase QTc interval. Contraindicated.

            • disopyramide

              disopyramide and nilotinib both increase QTc interval. Contraindicated.

            • goserelin

              goserelin increases toxicity of nilotinib by QTc interval. Contraindicated. Increases risk of torsades de pointes.

            • ibutilide

              ibutilide and nilotinib both increase QTc interval. Contraindicated.

            • indapamide

              indapamide and nilotinib both increase QTc interval. Contraindicated.

            • leuprolide

              leuprolide increases toxicity of nilotinib by QTc interval. Contraindicated. Increases risk of torsades de pointes.

            • pentamidine

              nilotinib and pentamidine both increase QTc interval. Contraindicated.

            • pimozide

              nilotinib and pimozide both increase QTc interval. Contraindicated.

              nilotinib increases levels of pimozide by decreasing metabolism. Contraindicated. Risk of QT interval prolongation.

            • procainamide

              nilotinib and procainamide both increase QTc interval. Contraindicated.

            • quinidine

              quinidine and nilotinib both increase QTc interval. Contraindicated.

            • sotalol

              nilotinib and sotalol both increase QTc interval. Contraindicated.

            • toremifene

              nilotinib and toremifene both increase QTc interval. Contraindicated. Avoid concurrent use of nilotinib with other QTc prolonging agents.

            Serious - Use Alternative (121)

            • abametapir

              abametapir will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.

            • afatinib

              nilotinib increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

            • alfuzosin

              alfuzosin and nilotinib both decrease QTc interval. Avoid or Use Alternate Drug.

            • amiodarone

              nilotinib will increase the level or effect of amiodarone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Additive QT prolongation may occur during coadministration of nilotinib and amiodarone Coadministration of nilotinib and a drug that prolongs the QT interval is not advised

              amiodarone and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • amitriptyline

              amitriptyline and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • amoxapine

              amoxapine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • apalutamide

              apalutamide will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.

            • apomorphine

              apomorphine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • aripiprazole

              aripiprazole and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • artemether

              artemether and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • artemether/lumefantrine

              artemether/lumefantrine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • atomoxetine

              atomoxetine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • bosutinib

              nilotinib increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • carbamazepine

              carbamazepine will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • chloramphenicol

              chloramphenicol will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • chlorpromazine

              chlorpromazine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • cimetidine

              cimetidine will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • clarithromycin

              clarithromycin will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              clarithromycin and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • clomipramine

              clomipramine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • deferiprone

              deferiprone, nilotinib. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid use of deferiprone with other drugs known to be associated with neutropenia or agranulocytosis; if an alternative is not possible, monitor absolute neutrophil count more frequently.

            • desipramine

              desipramine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • dexlansoprazole

              dexlansoprazole will decrease the level or effect of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Nilotinib has a pH-dependent solubility and solubility is decreased at higher pH; separating doses may not eliminate this effect because of PPI extended duration of action

            • dihydroergotamine

              nilotinib will increase the level or effect of dihydroergotamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • dihydroergotamine intranasal

              nilotinib will increase the level or effect of dihydroergotamine intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • disopyramide

              nilotinib will increase the level or effect of disopyramide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Additive QT prolongation may occur during coadministration of nilotinib and disopyramide Coadministration of nilotinib and a drug that prolongs the QT interval is not advised

            • dofetilide

              dofetilide and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • doxepin

              doxepin and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • dronedarone

              nilotinib will increase the level or effect of dronedarone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

              dronedarone and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • droperidol

              droperidol and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • edoxaban

              nilotinib will increase the level or effect of edoxaban by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Dose adjustment may be required with strong P-gp inhibitors. DVT/PE treatment: Decrease dose to 30 mg PO once daily. NVAF: No dose reduction recommended

            • encorafenib

              nilotinib will increase the level or effect of encorafenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use of a moderate CYP3A4 inhibitor is unavoidable, reduce encorafenib dose to one-half of the dose (eg, reduce from 450 mg/day to 225 mg/day). After discontinuing the inhibitor for 3-5 elimination half-lives, resume previous encorafenib dose.

              encorafenib and nilotinib both increase QTc interval. Avoid or Use Alternate Drug. Encorafenib is associated with dose-dependent QTc interval prolongation. Avoid with drugs known to prolong QT interval.

            • entrectinib

              nilotinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

            • enzalutamide

              enzalutamide will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • ergotamine

              nilotinib will increase the level or effect of ergotamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • eribulin

              eribulin and nilotinib both increase QTc interval. Avoid or Use Alternate Drug. Potential for enhanced QTc-prolonging effects; if concurrent use is necessary then ECG monitoring is recommended.

            • erythromycin base

              erythromycin base will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              nilotinib will increase the level or effect of erythromycin base by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

              erythromycin base and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • erythromycin ethylsuccinate

              erythromycin ethylsuccinate will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              erythromycin ethylsuccinate and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

              nilotinib will increase the level or effect of erythromycin ethylsuccinate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • erythromycin lactobionate

              erythromycin lactobionate will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              erythromycin lactobionate and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

              nilotinib will increase the level or effect of erythromycin lactobionate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • erythromycin stearate

              erythromycin stearate will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              erythromycin stearate and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

              nilotinib will increase the level or effect of erythromycin stearate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • escitalopram

              escitalopram increases toxicity of nilotinib by QTc interval. Avoid or Use Alternate Drug.

            • esomeprazole

              esomeprazole will decrease the level or effect of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Nilotinib has a pH-dependent solubility and solubility is decreased at higher pH; separating doses may not eliminate this effect because of PPI extended duration of action

            • everolimus

              nilotinib will increase the level or effect of everolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

              nilotinib will increase the level or effect of everolimus by P-glycoprotein (MDR1) efflux transporter. Contraindicated.

            • fexinidazole

              fexinidazole and nilotinib both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of fexinidazole with drugs known to block potassium channels and/or prolong QT interval.

              fexinidazole will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.

            • fluconazole

              fluconazole and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • fluphenazine

              fluphenazine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • formoterol

              formoterol and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • glasdegib

              nilotinib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.

            • haloperidol

              haloperidol and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • histrelin

              histrelin increases toxicity of nilotinib by QTc interval. Avoid or Use Alternate Drug. Increases risk of torsades de pointes.

            • hydroxychloroquine sulfate

              hydroxychloroquine sulfate and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • idelalisib

              idelalisib will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates

            • imipramine

              imipramine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • inotuzumab

              inotuzumab and nilotinib both increase QTc interval. Avoid or Use Alternate Drug. If unable to avoid concomitant use, obtain ECGs and electrolytes before and after initiation of any drug known to prolong QTc, and periodically monitor as clinically indicated during treatment.

            • isoniazid

              isoniazid will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • itraconazole

              itraconazole will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of a strong CYP3A4 inhibitor is unavoidable, reduce nilotinib to 300 mg qDay in patients with resistant or intolerant Ph+ CML or to 200 mg qDay in patients with newly diagnosed Ph+ CML-CP. If strong inhibitor is discontinued, allow a washout period before adjusting the nilotinib dose to the indicated dose.

              itraconazole and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • ivosidenib

              ivosidenib and nilotinib both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of QTc prolonging drugs with ivosidenib or replace with alternate therapies. If coadministration of a QTc prolonging drug is unavoidable, monitor for increased risk of QTc interval prolongation.

              ivosidenib will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternative therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.

            • ketoconazole

              ketoconazole will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              ketoconazole and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • lansoprazole

              lansoprazole will decrease the level or effect of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Nilotinib has a pH-dependent solubility and solubility is decreased at higher pH; separating doses may not eliminate this effect because of PPI extended duration of action

            • lasmiditan

              lasmiditan increases levels of nilotinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • lefamulin

              lefamulin and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • lofepramine

              lofepramine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • lonafarnib

              nilotinib will increase the level or effect of lonafarnib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of lonafarnib (a sensitive CYP3A substrate) with weak CYP3A inhibitors is unavoidable, reduce to, or continue lonafarnib at starting dose. Closely monitor for arrhythmias and events (eg, syncope, heart palpitations) since lonafarnib effect on QT interval is unknown.

            • lopinavir

              lopinavir will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • lovastatin

              nilotinib will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • lumefantrine

              lumefantrine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • macimorelin

              macimorelin and nilotinib both increase QTc interval. Avoid or Use Alternate Drug. Macimorelin causes an increase of ~11 msec in the corrected QT interval. Avoid coadministration with drugs that prolong QT interval, which could increase risk for developing torsade de pointes-type ventricular tachycardia. Allow sufficient washout time of drugs that are known to prolong the QT interval before administering macimorelin.

            • maprotiline

              maprotiline and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • mefloquine

              mefloquine increases toxicity of nilotinib by QTc interval. Avoid or Use Alternate Drug. Mefloquine may enhance the QTc prolonging effect of high risk QTc prolonging agents.

            • mifepristone

              mifepristone will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • moxifloxacin

              moxifloxacin and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • nefazodone

              nefazodone will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • nortriptyline

              nortriptyline and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • octreotide

              nilotinib and octreotide both increase QTc interval. Avoid or Use Alternate Drug.

            • octreotide (Antidote)

              nilotinib and octreotide (Antidote) both increase QTc interval. Avoid or Use Alternate Drug.

            • omeprazole

              omeprazole will decrease the level or effect of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Nilotinib has a pH-dependent solubility and solubility is decreased at higher pH; separating doses may not eliminate this effect because of PPI extended duration of action

            • ondansetron

              nilotinib and ondansetron both increase QTc interval. Avoid or Use Alternate Drug. Avoid with congenital long QT syndrome; ECG monitoring recommended with concomitant medications that prolong QT interval, electrolyte abnormalities, CHF, or bradyarrhythmias. Potential for increased ondansetron levels.

            • oxaliplatin

              oxaliplatin will increase the level or effect of nilotinib by Other (see comment). Avoid or Use Alternate Drug. Monitor for ECG changes if therapy is initiated in patients with drugs known to prolong QT interval.

            • palifermin

              palifermin increases toxicity of nilotinib by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hr before, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.

            • panobinostat

              nilotinib and panobinostat both increase QTc interval. Avoid or Use Alternate Drug. Panobinostat is known to significantly prolong QT interval. Panobinostat prescribing information states use with drugs known to prolong QTc is not recommended.

            • pantoprazole

              pantoprazole will decrease the level or effect of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Nilotinib has a pH-dependent solubility and solubility is decreased at higher pH; separating doses may not eliminate this effect because of PPI extended duration of action

            • pazopanib

              nilotinib will increase the level or effect of pazopanib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of pazopanib with strong CYP3A4 inhibitors if possible; if must coadminister, decrease pazopanib dose to 400 mg/day

            • perphenazine

              perphenazine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • pimavanserin

              nilotinib and pimavanserin both increase QTc interval. Avoid or Use Alternate Drug. Coadministration may increase the risk of QT prolongation and cardiac arrhythmia.

            • pitolisant

              nilotinib and pitolisant both increase QTc interval. Avoid or Use Alternate Drug.

            • pomalidomide

              nilotinib increases levels of pomalidomide by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • prochlorperazine

              prochlorperazine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • promazine

              promazine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • promethazine

              promethazine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • propafenone

              nilotinib will increase the level or effect of propafenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Additive QT prolongation may occur during coadministration of nilotinib and propafenone. Coadministration of nilotinib and a drug that prolongs the QT interval is not advised

            • protriptyline

              protriptyline and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • quinidine

              nilotinib will increase the level or effect of quinidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Additive QT prolongation may occur during coadministration of nilotinib and quinidine. Coadministration of nilotinib and a drug that prolongs the QT interval such as dronedarone is not advised

              quinidine will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • rabeprazole

              rabeprazole will decrease the level or effect of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Nilotinib has a pH-dependent solubility and solubility is decreased at higher pH; separating doses may not eliminate this effect because of PPI extended duration of action

            • ranolazine

              nilotinib will increase the level or effect of ranolazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • ribociclib

              ribociclib and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • rifabutin

              rifabutin will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • rifampin

              rifampin will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • riociguat

              nilotinib will increase the level or effect of riociguat by decreasing metabolism. Avoid or Use Alternate Drug. Coadministration of riociguat (substrate of CYP isoenzymes 1A1, 2C8, 3A, 2J2) with strong CYP inhibitors may require a decreased initial dose of 0.5 mg PO TID; monitor for signs of hypotension and reduce dose if needed

            • ritonavir

              ritonavir will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. May require decreased nilotinib dose or adjustment of dosing interval. Both ritonavir and nilotinib are CYP3A4 inhibitor, however, ritonavir is a strong CYP3A4 inhibitor and more likely to increase nilotinib levels and increase risk for toxicity including prolonged QT interval

            • saquinavir

              saquinavir will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • silodosin

              nilotinib will increase the level or effect of silodosin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • simvastatin

              nilotinib will increase the level or effect of simvastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • sirolimus

              nilotinib will increase the level or effect of sirolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • St John's Wort

              St John's Wort will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • tepotinib

              tepotinib will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If concomitant use unavoidable, reduce the P-gp substrate dosage if recommended in its approved product labeling.

            • thioridazine

              nilotinib will increase the level or effect of thioridazine by affecting hepatic enzyme CYP2D6 metabolism. Contraindicated.

              thioridazine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • tipranavir

              tipranavir will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • tolvaptan

              nilotinib will increase the level or effect of tolvaptan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • topotecan

              nilotinib will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Product labeling for PO topotecan recommends avoiding concomitant use of P-gp inhibitors; the interaction with IV topotecan may be less severe but is still likely of clinical significance

            • trazodone

              trazodone and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • trifluoperazine

              trifluoperazine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • trimipramine

              trimipramine and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.

            • triptorelin

              triptorelin increases toxicity of nilotinib by QTc interval. Avoid or Use Alternate Drug. Increases risk of torsades de pointes.

            • tucatinib

              nilotinib will increase the level or effect of tucatinib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of tucatinib (a CYP2C8 substrate) with a strong or moderate CYP2C8 inhibitors increases tucatinib plasma concentrations and risk of toxicities.

              tucatinib will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.

            • umeclidinium bromide/vilanterol inhaled

              nilotinib increases toxicity of umeclidinium bromide/vilanterol inhaled by QTc interval. Avoid or Use Alternate Drug. Exercise extreme caution when vilanterol coadministered with drugs that prolong QTc interval; adrenergic agonist effects on the cardiovascular system may be potentiated.

            • vandetanib

              nilotinib, vandetanib. Either increases toxicity of the other by QTc interval. Avoid or Use Alternate Drug. Avoid coadministration with drugs known to prolong QT interval; if a drug known to prolong QT interval must be used, more frequent ECG monitoring is recommended.

            • vemurafenib

              vemurafenib and nilotinib both increase QTc interval. Avoid or Use Alternate Drug. Concomitant use of vemurafenib with drugs that prolong QT interval is not recommended. Nilotinib may also increase vemurafenib levels.

            • venetoclax

              nilotinib will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.

            • vilanterol/fluticasone furoate inhaled

              nilotinib increases toxicity of vilanterol/fluticasone furoate inhaled by QTc interval. Avoid or Use Alternate Drug. Exercise extreme caution when vilanterol coadministered with drugs that prolong QTc interval; adrenergic agonist effects on the cardiovascular system may be potentiated.

            • vilazodone

              nilotinib increases levels of vilazodone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If intolerable adverse effects occur when coadministered with moderate CYP3A4 inhibitors, reduce daily dose to 20 mg.

            • voxelotor

              voxelotor will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.

            • ziprasidone

              nilotinib and ziprasidone both increase QTc interval. Avoid or Use Alternate Drug.

            Monitor Closely (286)

            • acalabrutinib

              acalabrutinib, nilotinib. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration may increase risk of myelosuppressive effects.

            • albuterol

              albuterol and nilotinib both increase QTc interval. Use Caution/Monitor.

            • alfuzosin

              nilotinib and alfuzosin both increase QTc interval. Use Caution/Monitor.

            • almotriptan

              nilotinib will increase the level or effect of almotriptan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • alprazolam

              nilotinib will increase the level or effect of alprazolam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • aluminum hydroxide

              aluminum hydroxide decreases levels of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Avoid this interaction by administering antacids 2 hr after or 2 hr before nilotinib.

            • aluminum hydroxide/magnesium carbonate

              aluminum hydroxide/magnesium carbonate decreases levels of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Avoid this interaction by administering antacids 2 hr after or 2 hr before nilotinib.

            • aluminum hydroxide/magnesium trisilicate

              aluminum hydroxide/magnesium trisilicate decreases levels of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Avoid this interaction by administering antacids 2 hr after or 2 hr before nilotinib.

            • amikacin

              nilotinib will increase the level or effect of amikacin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • amiodarone

              amiodarone will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • amlodipine

              nilotinib will increase the level or effect of amlodipine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • amobarbital

              amobarbital will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • aprepitant

              aprepitant will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • arformoterol

              arformoterol and nilotinib both increase QTc interval. Use Caution/Monitor.

            • aripiprazole

              nilotinib will increase the level or effect of aripiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • armodafinil

              armodafinil will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • artemether/lumefantrine

              nilotinib will increase the level or effect of artemether/lumefantrine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • aspirin/citric acid/sodium bicarbonate

              aspirin/citric acid/sodium bicarbonate decreases levels of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Avoid this interaction by administering antacids 2 hr after or 2 hr before nilotinib.

            • atazanavir

              atazanavir will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • atomoxetine

              nilotinib will increase the level or effect of atomoxetine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • atorvastatin

              nilotinib will increase the level or effect of atorvastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              atorvastatin will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • avanafil

              nilotinib will increase the level or effect of avanafil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. CYP3A4 inhibitors may reduce avanafil clearance increasing systemic exposure to avanafil; increased levels may result in increased associated adverse events; the maximum recommended dose of STENDRA is 50 mg, not to exceed once every 24 hours for patients taking concomitant moderate CYP3A4 inhibitors

            • avapritinib

              nilotinib will increase the level or effect of avapritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • azithromycin

              azithromycin and nilotinib both increase QTc interval. Use Caution/Monitor.

            • bazedoxifene/conjugated estrogens

              nilotinib will increase the level or effect of bazedoxifene/conjugated estrogens by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of bazedoxifene/conjugated estrogens by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • bedaquiline

              nilotinib and bedaquiline both increase QTc interval. Modify Therapy/Monitor Closely. ECG should be monitored closely

            • benzhydrocodone/acetaminophen

              nilotinib will increase the level or effect of benzhydrocodone/acetaminophen by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Hydromorphone (<3% of the circulating parent hydrocodone [benzhydrocodone is prodrug of hydrocodone]) is mainly formed by CYP2D6 mediated O-demethylation of hydrocodone. Hydromorphone may contribute to the total analgesic effect of hydrocodone.

            • berotralstat

              berotralstat will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor or titrate P-gp substrate dose if coadministered.

            • betrixaban

              nilotinib increases levels of betrixaban by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Decrease betrixaban dose to 80 mg PO once, then 40 mg PO qDay if coadministered with a P-gp inhibitor.

            • bexarotene

              nilotinib will increase the level or effect of bexarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • bosentan

              bosentan will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • budesonide

              nilotinib will increase the level or effect of budesonide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              budesonide will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of budesonide by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • bupropion

              nilotinib, bupropion. increasing metabolism. Use Caution/Monitor. Decr levels of bupropion, but incr levels of active metabolites. .

            • buspirone

              nilotinib will increase the level or effect of buspirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • butabarbital

              butabarbital will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • butalbital

              butalbital will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • calcium carbonate

              calcium carbonate decreases levels of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Avoid this interaction by administering antacids 2 hr after or 2 hr before nilotinib.

            • carbamazepine

              nilotinib will increase the level or effect of carbamazepine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • carvedilol

              nilotinib will increase the level or effect of carvedilol by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of carvedilol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • cenobamate

              cenobamate will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.

            • ceritinib

              nilotinib increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • chloroquine

              chloroquine increases toxicity of nilotinib by QTc interval. Use Caution/Monitor.

            • cilostazol

              nilotinib will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • cimetidine

              cimetidine decreases levels of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Avoid this interaction by administering H2 antagonists 10 hr after or 2 hr before nilotinib.

            • cinacalcet

              nilotinib will increase the level or effect of cinacalcet by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • ciprofloxacin

              ciprofloxacin and nilotinib both increase QTc interval. Use Caution/Monitor. Ciprofloxacin elicits minimal effects on QT interval. Caution if used in combination with other drugs known to affect QT interval or in patients with other risk factors.

            • citalopram

              nilotinib and citalopram both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended, along with drugs that may prolong the QT interval.

            • citric acid/sodium bicarbonate

              citric acid/sodium bicarbonate decreases levels of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Avoid this interaction by administering antacids 2 hr after or 2 hr before nilotinib.

            • clarithromycin

              clarithromycin will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • clobetasone

              nilotinib will increase the level or effect of clobetasone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of clobetasone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • clomipramine

              nilotinib will increase the level or effect of clomipramine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • clopidogrel

              nilotinib will decrease the level or effect of clopidogrel by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Inhibition of CYP3A4 will reduce clopidogrel bioactivation

            • clotrimazole

              clotrimazole will decrease the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • clozapine

              nilotinib will increase the level or effect of clozapine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • cobicistat

              cobicistat will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Dosage adjustment of nilotinib may be necessary upon coadministration with cobicistat coadministered with atazanavir or darunavir. Refer nilotinib prescribing information for dosing instructions.

            • conivaptan

              conivaptan will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • conjugated estrogens

              nilotinib will increase the level or effect of conjugated estrogens by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of conjugated estrogens by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • conjugated estrogens, vaginal

              nilotinib will increase the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • cortisone

              nilotinib will increase the level or effect of cortisone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              cortisone will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of cortisone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • crizotinib

              crizotinib increases levels of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Dose reduction may be needed for coadministered drugs that are predominantly metabolized by CYP3A. ECG monitoring is recommended, along with drugs that may prolong the QT interval.

            • crofelemer

              crofelemer increases levels of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Crofelemer has the potential to inhibit CYP3A4 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.

            • cyclosporine

              nilotinib will increase the level or effect of cyclosporine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              cyclosporine will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • dabigatran

              nilotinib will increase the level or effect of dabigatran by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Atrial fibrillation: Avoid coadministering dabigatran with P-gp inhibitors if CrCl <30 mL/min. DVT/PE treatment: Avoid coadministering dabigatran with P-gp inhibitors if CrCl <50 mL/min

            • dabrafenib

              dabrafenib will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.

            • darifenacin

              darifenacin will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of darifenacin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • darunavir

              darunavir will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Nilotinib may require adjustment of dose or dosing interval if coadministered.

            • dasatinib

              dasatinib will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              dasatinib and nilotinib both increase QTc interval. Modify Therapy/Monitor Closely.

            • daunorubicin

              nilotinib will increase the level or effect of daunorubicin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • deferasirox

              deferasirox will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • deflazacort

              nilotinib will increase the level or effect of deflazacort by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Decrease deflazacort dose to one-third of the recommended dose if coadministered with moderate or strong CYP3A4 inhibitors.

              nilotinib will increase the level or effect of deflazacort by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • desipramine

              nilotinib will increase the level or effect of desipramine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • deutetrabenazine

              nilotinib and deutetrabenazine both increase QTc interval. Modify Therapy/Monitor Closely. For patients requiring deutetrabenazine doses >24 mg/day and are taking other drugs known to prolong QTc, assess the QTc interval before and after increasing the dose of deutetrabenazine or other medications known to prolong QTc.

            • dexamethasone

              nilotinib will increase the level or effect of dexamethasone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              dexamethasone will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of dexamethasone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • DHEA, herbal

              DHEA, herbal will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • diazepam

              nilotinib will increase the level or effect of diazepam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • dichlorphenamide

              dichlorphenamide and nilotinib both decrease serum potassium. Use Caution/Monitor.

            • dienogest/estradiol valerate

              nilotinib will increase the level or effect of dienogest/estradiol valerate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Monitor for potential adverse effects such as nausea, irregular uterine bleeding, breast tenderness and headache.

            • digoxin

              nilotinib will increase the level or effect of digoxin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • diltiazem

              diltiazem will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of diltiazem by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • docetaxel

              nilotinib will increase the level or effect of docetaxel by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • dolasetron

              dolasetron and nilotinib both increase QTc interval. Modify Therapy/Monitor Closely.

            • doxepin

              nilotinib will increase the level or effect of doxepin by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • doxorubicin

              nilotinib will increase the level or effect of doxorubicin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of doxorubicin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • doxorubicin liposomal

              nilotinib will increase the level or effect of doxorubicin liposomal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of doxorubicin liposomal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • dronedarone

              dronedarone will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              dronedarone will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Avoid concurrent use of nilotinib with other QTc-prolonging agents. Coadministration with other agents that can prolong QT interval may result in additive effects and increased risk of ventricular arrhythmias including torsade de pointes.

            • duloxetine

              nilotinib will increase the level or effect of duloxetine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • duvelisib

              duvelisib will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration with duvelisib increases AUC of a sensitive CYP3A4 substrate which may increase the risk of toxicities of these drugs. Consider reducing the dose of the sensitive CYP3A4 substrate and monitor for signs of toxicities of the coadministered sensitive CYP3A substrate.

            • efavirenz

              efavirenz will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • elagolix

              elagolix will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              elagolix decreases levels of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.

            • eletriptan

              nilotinib will increase the level or effect of eletriptan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • eliglustat

              eliglustat increases levels of nilotinib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Monitor therapeutic drug concentrations, as indicated, or consider reducing the dosage of the P-gp substrate and titrate to clinical effect.

            • elvitegravir/cobicistat/emtricitabine/tenofovir DF

              elvitegravir/cobicistat/emtricitabine/tenofovir DF increases levels of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Cobicistat is a CYP3A4 inhibitor; contraindicated with CYP3A4 substrates for which elevated plasma concentrations are associated with serious and/or life-threatening events.

            • encorafenib

              encorafenib, nilotinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.

            • erlotinib

              nilotinib will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • erythromycin base

              erythromycin base will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • erythromycin ethylsuccinate

              erythromycin ethylsuccinate will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • erythromycin lactobionate

              erythromycin lactobionate will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • erythromycin stearate

              erythromycin stearate will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • eslicarbazepine acetate

              eslicarbazepine acetate will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • estradiol

              nilotinib will increase the level or effect of estradiol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of estradiol by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • estrogens conjugated synthetic

              nilotinib will increase the level or effect of estrogens conjugated synthetic by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of estrogens conjugated synthetic by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • estropipate

              nilotinib will increase the level or effect of estropipate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of estropipate by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • ethinylestradiol

              ethinylestradiol will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • etonogestrel

              nilotinib will increase the level or effect of etonogestrel by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • etoposide

              nilotinib will increase the level or effect of etoposide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of etoposide by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • etravirine

              nilotinib will increase the level or effect of etravirine by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of etravirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              etravirine will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • ezogabine

              ezogabine, nilotinib. Either increases toxicity of the other by QTc interval. Use Caution/Monitor. Slight and transient QT-prolongation observed with ezogabine, particularly when dose titrated to 1200 mg/day. QT interval should be monitored when ezogabine is prescribed with agents known to increase QT interval.

            • famotidine

              famotidine decreases levels of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Avoid this interaction by administering H2 antagonists 10 hr after or 2 hr before nilotinib.

            • fedratinib

              fedratinib will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.

            • felodipine

              nilotinib will increase the level or effect of felodipine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              felodipine will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • fesoterodine

              nilotinib will increase the level or effect of fesoterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • finerenone

              nilotinib will increase the level or effect of finerenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor serum potassium during initiation and dosage adjustment of either finererone or weak CYP3A4 inhibitors. Adjust finererone dosage as needed.

            • flecainide

              nilotinib will increase the level or effect of flecainide by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

              flecainide and nilotinib both increase QTc interval. Modify Therapy/Monitor Closely.

            • fluconazole

              fluconazole will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • fludrocortisone

              nilotinib will increase the level or effect of fludrocortisone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of fludrocortisone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • fluoxetine

              fluoxetine and nilotinib both increase QTc interval. Modify Therapy/Monitor Closely.

            • fluvoxamine

              fluvoxamine will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • fosamprenavir

              fosamprenavir will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • foscarnet

              foscarnet and nilotinib both increase QTc interval. Modify Therapy/Monitor Closely.

            • fosphenytoin

              nilotinib will increase the level or effect of fosphenytoin by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

              fosphenytoin will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              fosphenytoin will decrease the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • fostemsavir

              nilotinib and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir.

            • gemtuzumab

              nilotinib and gemtuzumab both increase QTc interval. Use Caution/Monitor.

            • gentamicin

              nilotinib will increase the level or effect of gentamicin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • glecaprevir/pibrentasvir

              nilotinib will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              glecaprevir/pibrentasvir will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • grapefruit

              grapefruit will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • griseofulvin

              griseofulvin will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • guanfacine

              nilotinib will increase the level or effect of guanfacine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Strong or moderate CYP3A4 inhibitors significantly increase guanfacine plasma concentrations. FDA-approved labeling for extended-release (ER) guanfacine recommends that, if coadministered, the guanfacine dosage should be decreased to half of the recommended dose. Specific recommendations for immediate-release (IR) guanfacine are not available.

            • haloperidol

              nilotinib will increase the level or effect of haloperidol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • hydrocodone

              nilotinib will increase the level or effect of hydrocodone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Hydromorphone (<3% of the circulating parent hydrocodone) is mainly formed by CYP2D6 mediated O-demethylation of hydrocodone. Hydromorphone may contribute to the total analgesic effect of hydrocodone.

            • hydrocortisone

              nilotinib will increase the level or effect of hydrocortisone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of hydrocortisone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • hydroxyprogesterone caproate

              nilotinib will increase the level or effect of hydroxyprogesterone caproate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • ibuprofen/famotidine

              ibuprofen/famotidine decreases levels of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Avoid this interaction by administering H2 antagonists 10 hr after or 2 hr before nilotinib.

            • ifosfamide

              nilotinib increases effects of ifosfamide by affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor. Coadministration of ifosfamide with CYP2B6 inducers may increase metabolism of ifosfamide to its metabolite. Monitor for increased effects/toxicities if combined with CYP2B6 inducers.

              nilotinib decreases effects of ifosfamide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Use of a CYP3A4 inhibitor may decrease metabolism of ifosfamide, potentially reducing ifosfamide therapeutic effects.

            • iloperidone

              nilotinib will increase the level or effect of iloperidone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

              iloperidone and nilotinib both increase QTc interval. Modify Therapy/Monitor Closely.

              iloperidone increases levels of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Iloperidone is a time-dependent CYP3A inhibitor and may lead to increased plasma levels of drugs predominantly eliminated by CYP3A4.

            • imatinib

              nilotinib will increase the level or effect of imatinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • imipramine

              nilotinib will increase the level or effect of imipramine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • indacaterol, inhaled

              indacaterol, inhaled, nilotinib. QTc interval. Use Caution/Monitor. Drugs that are known to prolong the QTc interval may have an increased the risk of ventricular arrhythmias.

            • indinavir

              indinavir will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of indinavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              indinavir will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • irinotecan

              nilotinib will increase the level or effect of irinotecan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • irinotecan liposomal

              nilotinib will increase the level or effect of irinotecan liposomal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • istradefylline

              istradefylline will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.

              istradefylline will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of P-gp substrates in clinical trials. Consider dose reduction of sensitive P-gp substrates.

            • ivacaftor

              ivacaftor increases levels of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Ivacaftor and its M1 metabolite has the potential to inhibit P-gp; may significantly increase systemic exposure to sensitive P-gp substrates with a narrow therapeutic index.

            • ivermectin

              nilotinib will increase the level or effect of ivermectin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • ivosidenib

              nilotinib will increase the level or effect of ivosidenib by affecting hepatic enzyme CYP2E1 metabolism. Use Caution/Monitor. Coadministration with moderate CYP3A4 inhibitors may increase ivosidenib plasma concentrations, thus increasing the risk of QTc prolongation. Monitor for increased risk of QTc interval prolongation.

            • ixabepilone

              nilotinib will increase the level or effect of ixabepilone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • ketoconazole

              ketoconazole will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • lapatinib

              lapatinib will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              lapatinib will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              lapatinib and nilotinib both increase QTc interval. Modify Therapy/Monitor Closely.

            • lemborexant

              nilotinib will increase the level or effect of lemborexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Lower nightly dose of lemborexant recommended if coadministered with weak CYP3A4 inhibitors. See drug monograph for specific dosage modification.

            • lenvatinib

              nilotinib and lenvatinib both increase QTc interval. Use Caution/Monitor. Lenvatinib prescribing information recommends monitoring ECG closely when coadministered with QT prolonging drugs.

            • levofloxacin

              levofloxacin and nilotinib both increase QTc interval. Modify Therapy/Monitor Closely.

            • lofexidine

              nilotinib and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

            • lomitapide

              nilotinib increases levels of lomitapide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lomitapide dose should not exceed 30 mg/day.

            • lonafarnib

              lonafarnib will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Lonafarnib is a weak P-gp inhibitor. Monitor for adverse reactions if coadministered with P-gp substrates where minimal concentration changes may lead to serious or life-threatening toxicities. Reduce P-gp substrate dose if needed.

            • loperamide

              nilotinib will increase the level or effect of loperamide by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • lopinavir

              nilotinib will increase the level or effect of lopinavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • loratadine

              nilotinib will increase the level or effect of loratadine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              loratadine will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • lorlatinib

              lorlatinib will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • lovastatin

              lovastatin will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • lumefantrine

              nilotinib will increase the level or effect of lumefantrine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • lurasidone

              nilotinib increases levels of lurasidone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Manufacturer recommends decreasing starting dose of lurasidone to 20 mg/day and maximum daily dose of lurasidone 80 mg when coadministered with moderate CYP3A4 inhibitors. Concurrent use may increase risk of lurasidone-related adverse reactions.

            • magnesium oxide

              magnesium oxide decreases levels of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Avoid this interaction by administering antacids 2 hr after or 2 hr before nilotinib.

            • maraviroc

              nilotinib will increase the level or effect of maraviroc by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of maraviroc by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • marijuana

              marijuana will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • mestranol

              nilotinib will increase the level or effect of mestranol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of mestranol by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • metformin

              nilotinib decreases effects of metformin by pharmacodynamic antagonism. Use Caution/Monitor.

            • methadone

              nilotinib will increase the level or effect of methadone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              methadone and nilotinib both increase QTc interval. Modify Therapy/Monitor Closely.

            • methamphetamine

              nilotinib will increase the level or effect of methamphetamine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • methylprednisolone

              nilotinib will increase the level or effect of methylprednisolone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of methylprednisolone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • metoprolol

              nilotinib will increase the level or effect of metoprolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • metronidazole

              metronidazole will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • mexiletine

              nilotinib will increase the level or effect of mexiletine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • miconazole vaginal

              miconazole vaginal will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • midazolam

              nilotinib will increase the level or effect of midazolam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • midazolam intranasal

              nilotinib will increase the level or effect of midazolam intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of mild CYP3A4 inhibitors with midazolam intranasal may cause higher midazolam systemic exposure, which may prolong sedation.

            • mifepristone

              mifepristone, nilotinib. QTc interval. Modify Therapy/Monitor Closely. Use alternatives if available.

            • mitotane

              mitotane decreases levels of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.

            • modafinil

              modafinil will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • morphine

              nilotinib will increase the level or effect of morphine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • nafcillin

              nafcillin will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • naldemedine

              nilotinib increases levels of naldemedine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor naldemedine for potential adverse effects if coadministered with P-gp inhibitors.

            • nateglinide

              nilotinib will increase the level or effect of nateglinide by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

            • nebivolol

              nilotinib will increase the level or effect of nebivolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • nefazodone

              nefazodone will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • nelfinavir

              nelfinavir will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of nelfinavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of nelfinavir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • neomycin PO

              nilotinib will increase the level or effect of neomycin PO by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • nevirapine

              nevirapine will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nicardipine

              nilotinib will increase the level or effect of nicardipine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nicardipine will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • nifedipine

              nifedipine will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nifedipine will decrease the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • nintedanib

              nilotinib increases levels of nintedanib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. If nintedanib adverse effects occur, management may require interruption, dose reduction, or discontinuation of therapy.

            • nisoldipine

              nilotinib will increase the level or effect of nisoldipine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nizatidine

              nizatidine decreases levels of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Avoid this interaction by administering H2 antagonists 10 hr after or 2 hr before nilotinib.

            • nortriptyline

              nilotinib will increase the level or effect of nortriptyline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • ofatumumab SC

              ofatumumab SC, nilotinib. Either increases effects of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Consider the risk of additive immune system effects when coadministering immunosuppressive therapies with coadministration. When switching from therapies with immune effects, take into account the duration and mechanism of action of these therapies when initiating ofatumumab SC.

            • ofloxacin

              nilotinib and ofloxacin both increase QTc interval. Modify Therapy/Monitor Closely.

            • olodaterol inhaled

              nilotinib and olodaterol inhaled both increase QTc interval. Use Caution/Monitor. Drugs that prolong the QTc interval and may potentiate the effects of beta2 agonists on the cardiovascular system; increased risk of ventricular arrhythmias

            • osilodrostat

              osilodrostat and nilotinib both increase QTc interval. Use Caution/Monitor.

            • osimertinib

              osimertinib and nilotinib both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.

            • oxcarbazepine

              oxcarbazepine will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • oxycodone

              nilotinib will increase the level or effect of oxycodone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • ozanimod

              ozanimod and nilotinib both increase QTc interval. Modify Therapy/Monitor Closely. The potential additive effects on heart rate, treatment with ozanimod should generally not be initiated in patients who are concurrently treated with QT prolonging drugs with known arrhythmogenic properties.

            • paclitaxel

              nilotinib will increase the level or effect of paclitaxel by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • paclitaxel protein bound

              nilotinib will increase the level or effect of paclitaxel protein bound by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • paliperidone

              nilotinib will increase the level or effect of paliperidone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              nilotinib and paliperidone both increase QTc interval. Modify Therapy/Monitor Closely.

            • paroxetine

              nilotinib and paroxetine both increase QTc interval. Modify Therapy/Monitor Closely.

            • pasireotide

              nilotinib and pasireotide both increase QTc interval. Modify Therapy/Monitor Closely.

            • pazopanib

              nilotinib and pazopanib both increase QTc interval. Use Caution/Monitor.

            • pentobarbital

              pentobarbital will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • phenobarbital

              phenobarbital will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              phenobarbital will decrease the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • phenytoin

              nilotinib will increase the level or effect of phenytoin by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. Avoid concomitant use of phenytoin with nilotinib.

              phenytoin will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              phenytoin will decrease the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. A reduction in therapeutic effectiveness of nilotinib may occur. Concomitant use of phenytoin with lapatinib, nilotinib, lapatinib, or pazopanib should be avoided.

            • ponatinib

              ponatinib increases levels of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • posaconazole

              posaconazole will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of posaconazole by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              nilotinib and posaconazole both increase QTc interval. Modify Therapy/Monitor Closely.

            • prednisolone

              nilotinib will increase the level or effect of prednisolone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • prednisone

              nilotinib will increase the level or effect of prednisone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of prednisone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • primidone

              primidone will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • propafenone

              nilotinib will increase the level or effect of propafenone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • propranolol

              nilotinib will increase the level or effect of propranolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • quercetin

              quercetin will decrease the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • quetiapine

              nilotinib will increase the level or effect of quetiapine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              quetiapine, nilotinib. Either increases toxicity of the other by QTc interval. Use Caution/Monitor. Avoid use with drugs that prolong QT and in patients with risk factors for prolonged QT interval. Postmarketing cases show QT prolongation with overdose in patients with concomitant illness or with drugs known to cause electrolyte imbalance or prolong QT.

            • quinine

              nilotinib and quinine both increase QTc interval. Use Caution/Monitor.

            • quinupristin/dalfopristin

              quinupristin/dalfopristin will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • ranolazine

              ranolazine will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              nilotinib and ranolazine both increase QTc interval. Modify Therapy/Monitor Closely.

            • repaglinide

              nilotinib will increase the level or effect of repaglinide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • ribociclib

              ribociclib will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.

            • rifampin

              rifampin will decrease the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • rifapentine

              rifapentine will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • rifaximin

              nilotinib increases levels of rifaximin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • rilpivirine

              rilpivirine increases toxicity of nilotinib by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.

            • risperidone

              nilotinib and risperidone both increase QTc interval. Modify Therapy/Monitor Closely.

            • ritonavir

              nilotinib will increase the level or effect of ritonavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of ritonavir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • rivaroxaban

              nilotinib increases levels of rivaroxaban by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Patients with renal impairment receiving rivaroxaban with drugs that are combined P-gp and weak or moderate CYP3A4 inhibitors may have significant increases in exposure compared with patients with normal renal function and no inhibitor use, since both pathways of rivaroxaban elimination are affected. Since these increases may increase bleeding risk, use rivaroxaban in this situation only if the potential benefit justifies the potential risk.

            • romidepsin

              nilotinib will increase the level or effect of romidepsin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of romidepsin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              nilotinib and romidepsin both increase QTc interval. Modify Therapy/Monitor Closely.

            • rucaparib

              rucaparib will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.

            • rufinamide

              rufinamide will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • saquinavir

              nilotinib will increase the level or effect of saquinavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of saquinavir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • sarecycline

              sarecycline will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor for toxicities of P-gp substrates that may require dosage reduction when coadministered with P-gp inhibitors.

            • secobarbital

              secobarbital will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • selexipag

              nilotinib will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.

            • selpercatinib

              selpercatinib increases toxicity of nilotinib by QTc interval. Use Caution/Monitor.

            • sildenafil

              nilotinib will increase the level or effect of sildenafil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • silodosin

              nilotinib will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • siponimod

              siponimod and nilotinib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.

            • sirolimus

              nilotinib will increase the level or effect of sirolimus by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • sodium sulfate/?magnesium sulfate/potassium chloride

              sodium sulfate/?magnesium sulfate/potassium chloride increases toxicity of nilotinib by QTc interval. Use Caution/Monitor. Consider predose and post-colonoscopy ECGs in patients at increased risk of serious cardiac arrhythmias. .

            • sodium sulfate/potassium sulfate/magnesium sulfate

              sodium sulfate/potassium sulfate/magnesium sulfate increases toxicity of nilotinib by QTc interval. Use Caution/Monitor. Consider predose and post-colonoscopy ECGs in patients at increased risk of serious cardiac arrhythmias. .

            • sodium zirconium cyclosilicate

              sodium zirconium cyclosilicate will decrease the level or effect of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Check specific recommendations for drugs that exhibit pH-dependent solubility that may affect their systemic exposure and efficacy. In general, administer drugs at least 2 hr before or after sodium zirconium cyclosilicate.

            • solifenacin

              nilotinib will increase the level or effect of solifenacin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • sorafenib

              sorafenib and nilotinib both increase QTc interval. Use Caution/Monitor.

            • St John's Wort

              St John's Wort will decrease the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • stiripentol

              stiripentol, nilotinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.

              stiripentol will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Consider reducing the dose of P-glycoprotein (P-gp) substrates, if adverse reactions are experienced when administered concomitantly with stiripentol.

            • streptomycin

              nilotinib will increase the level or effect of streptomycin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • sulfamethoxazole

              sulfamethoxazole and nilotinib both increase QTc interval. Modify Therapy/Monitor Closely.

            • sunitinib

              nilotinib will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tacrolimus

              nilotinib will increase the level or effect of tacrolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of tacrolimus by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • tadalafil

              nilotinib will increase the level or effect of tadalafil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tamoxifen

              nilotinib, tamoxifen. affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. CYP2C9/10 inhibition decreases tamoxifen metabolism to active metabolites.

              nilotinib, tamoxifen. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. CYP3A4 inhibition decreases metabolism of tamoxifen to N-desmethyl tamoxifen (active metabolite with similar biologic activity).

            • tazemetostat

              tazemetostat will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of tazemetostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tecovirimat

              tecovirimat will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.

            • telavancin

              nilotinib and telavancin both increase QTc interval. Modify Therapy/Monitor Closely.

            • temsirolimus

              nilotinib will increase the level or effect of temsirolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • teniposide

              nilotinib will increase the level or effect of teniposide by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • theophylline

              nilotinib will increase the level or effect of theophylline by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • timolol

              nilotinib will increase the level or effect of timolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • tinidazole

              nilotinib will increase the level or effect of tinidazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tipranavir

              nilotinib will increase the level or effect of tipranavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tobramycin

              nilotinib will increase the level or effect of tobramycin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • tolterodine

              nilotinib will increase the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tolvaptan

              nilotinib will increase the level or effect of tolvaptan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • topiramate

              topiramate will decrease the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • trastuzumab

              trastuzumab, nilotinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .

            • trastuzumab deruxtecan

              trastuzumab deruxtecan, nilotinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .

            • trazodone

              nilotinib will increase the level or effect of trazodone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              trazodone will decrease the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • triamcinolone acetonide injectable suspension

              nilotinib will increase the level or effect of triamcinolone acetonide injectable suspension by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • triazolam

              nilotinib will increase the level or effect of triazolam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • triclabendazole

              triclabendazole and nilotinib both increase QTc interval. Use Caution/Monitor.

            • tropisetron

              nilotinib and tropisetron both increase QTc interval. Modify Therapy/Monitor Closely.

            • tucatinib

              tucatinib will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Consider reducing the dosage of P-gp substrates, where minimal concentration changes may lead to serious or life-threatening toxicities.

            • vardenafil

              nilotinib will increase the level or effect of vardenafil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • venlafaxine

              nilotinib and venlafaxine both increase QTc interval. Modify Therapy/Monitor Closely.

            • verapamil

              nilotinib will increase the level or effect of verapamil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              verapamil will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • vinblastine

              nilotinib will increase the level or effect of vinblastine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • vincristine

              nilotinib will increase the level or effect of vincristine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • vincristine liposomal

              nilotinib will increase the level or effect of vincristine liposomal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • voclosporin

              voclosporin, nilotinib. Either increases effects of the other by QTc interval. Use Caution/Monitor.

            • voriconazole

              voriconazole will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              nilotinib and voriconazole both increase QTc interval. Modify Therapy/Monitor Closely.

            • warfarin

              nilotinib will increase the level or effect of warfarin by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

              nilotinib will increase the level or effect of warfarin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • zafirlukast

              zafirlukast will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            Minor (77)

            • alfentanil

              nilotinib will increase the level or effect of alfentanil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • alfuzosin

              nilotinib will increase the level or effect of alfuzosin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • aliskiren

              nilotinib will increase the level or effect of aliskiren by P-glycoprotein (MDR1) efflux transporter. Minor/Significance Unknown.

            • alosetron

              nilotinib will increase the level or effect of alosetron by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.

              nilotinib will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • alvimopan

              nilotinib will increase the level or effect of alvimopan by P-glycoprotein (MDR1) efflux transporter. Minor/Significance Unknown.

            • amitriptyline

              nilotinib will increase the level or effect of amitriptyline by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • aripiprazole

              nilotinib will increase the level or effect of aripiprazole by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

            • armodafinil

              nilotinib will increase the level or effect of armodafinil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • atazanavir

              nilotinib will increase the level or effect of atazanavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • bosentan

              nilotinib will increase the level or effect of bosentan by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.

              nilotinib will increase the level or effect of bosentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • celecoxib

              nilotinib will increase the level or effect of celecoxib by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.

            • cevimeline

              nilotinib will increase the level or effect of cevimeline by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • chlorpromazine

              nilotinib will increase the level or effect of chlorpromazine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

            • clarithromycin

              nilotinib will increase the level or effect of clarithromycin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • clomipramine

              nilotinib will increase the level or effect of clomipramine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • cocaine

              nilotinib will decrease the level or effect of cocaine by affecting hepatic enzyme CYP2B6 metabolism. Minor/Significance Unknown.

            • codeine

              nilotinib will increase the level or effect of codeine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

            • dapsone

              nilotinib will increase the level or effect of dapsone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • desipramine

              nilotinib will increase the level or effect of desipramine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • dextromethorphan

              nilotinib will increase the level or effect of dextromethorphan by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

            • diclofenac

              nilotinib will increase the level or effect of diclofenac by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.

            • docetaxel

              nilotinib will increase the level or effect of docetaxel by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • donepezil

              nilotinib will increase the level or effect of donepezil by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

              nilotinib will increase the level or effect of donepezil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • dutasteride

              nilotinib will increase the level or effect of dutasteride by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • efavirenz

              nilotinib will increase the level or effect of efavirenz by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • eplerenone

              nilotinib will increase the level or effect of eplerenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • eucalyptus

              nilotinib will increase the level or effect of eucalyptus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • fesoterodine

              nilotinib will increase the level or effect of fesoterodine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

            • fexofenadine

              nilotinib will increase the level or effect of fexofenadine by P-glycoprotein (MDR1) efflux transporter. Minor/Significance Unknown.

            • finasteride

              nilotinib will increase the level or effect of finasteride by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • fluoxetine

              nilotinib will increase the level or effect of fluoxetine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

            • fluphenazine

              nilotinib will increase the level or effect of fluphenazine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

            • flurbiprofen

              nilotinib will increase the level or effect of flurbiprofen by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.

            • fluvastatin

              nilotinib will increase the level or effect of fluvastatin by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.

            • galantamine

              nilotinib will increase the level or effect of galantamine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

              nilotinib will increase the level or effect of galantamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • ibuprofen

              nilotinib will increase the level or effect of ibuprofen by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.

            • ibuprofen IV

              nilotinib will increase the level or effect of ibuprofen IV by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.

            • imatinib

              nilotinib will increase the level or effect of imatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • imipramine

              nilotinib will increase the level or effect of imipramine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • isradipine

              nilotinib will increase the level or effect of isradipine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • itraconazole

              nilotinib will increase the level or effect of itraconazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • ketoconazole

              nilotinib will increase the level or effect of ketoconazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • loratadine

              nilotinib will increase the level or effect of loratadine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

              nilotinib will increase the level or effect of loratadine by P-glycoprotein (MDR1) efflux transporter. Minor/Significance Unknown.

            • meloxicam

              nilotinib will increase the level or effect of meloxicam by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.

            • montelukast

              nilotinib will increase the level or effect of montelukast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • nifedipine

              nilotinib will increase the level or effect of nifedipine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • nimodipine

              nilotinib will increase the level or effect of nimodipine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • nitrendipine

              nilotinib will increase the level or effect of nitrendipine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • oxybutynin

              nilotinib will increase the level or effect of oxybutynin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • paclitaxel

              nilotinib will increase the level or effect of paclitaxel by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • paclitaxel protein bound

              nilotinib will increase the level or effect of paclitaxel protein bound by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • parecoxib

              nilotinib will increase the level or effect of parecoxib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • paroxetine

              nilotinib will increase the level or effect of paroxetine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

            • perphenazine

              nilotinib will increase the level or effect of perphenazine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

            • pimozide

              nilotinib will increase the level or effect of pimozide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • pioglitazone

              nilotinib will increase the level or effect of pioglitazone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • piroxicam

              nilotinib will increase the level or effect of piroxicam by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.

            • prochlorperazine

              nilotinib will increase the level or effect of prochlorperazine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

            • promethazine

              nilotinib will increase the level or effect of promethazine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

            • quinine

              nilotinib will increase the level or effect of quinine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • ramelteon

              nilotinib will increase the level or effect of ramelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • risperidone

              nilotinib will increase the level or effect of risperidone by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

            • saxagliptin

              nilotinib will increase the level or effect of saxagliptin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • sufentanil

              nilotinib will increase the level or effect of sufentanil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • sulfamethoxazole

              nilotinib will increase the level or effect of sulfamethoxazole by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.

            • tolbutamide

              nilotinib will increase the level or effect of tolbutamide by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.

            • tolterodine

              nilotinib will increase the level or effect of tolterodine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

            • tramadol

              nilotinib will increase the level or effect of tramadol by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

            • trifluoperazine

              nilotinib will increase the level or effect of trifluoperazine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.

            • vinblastine

              nilotinib will increase the level or effect of vinblastine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • vincristine

              nilotinib will increase the level or effect of vincristine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • vincristine liposomal

              nilotinib will increase the level or effect of vincristine liposomal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • voriconazole

              nilotinib will increase the level or effect of voriconazole by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.

            • zaleplon

              nilotinib will increase the level or effect of zaleplon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • ziprasidone

              nilotinib will increase the level or effect of ziprasidone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • zolpidem

              nilotinib will increase the level or effect of zolpidem by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • zonisamide

              nilotinib will increase the level or effect of zonisamide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            Previous
            Next:

            Adverse Effects

            >10%

            Rash (33%)

            Headache (31%)

            Nausea (31%)

            Pruritus (29%)

            Fatigue (28%)

            Pyrexia (24%)

            Diarrhea (22%)

            Constipation (21%)

            Vomiting (21%)

            Arthralgia (18%)

            Cough (17%)

            Extremity pain (16%)

            Asthenia (14%)

            Muscle spasms (14%)

            Myalgia (14%)

            Abdominal pain (13%)

            Bone pain (13%)

            Back pain (12%)

            Dyspnea (11%)

            Nasopharyngitis (11%)

            Peripheral edema (11%)

            1-10% (selected)

            Dizziness

            Insomnia

            Paresthesia

            QT interval prolongation

            HTN

            Palpitations

            QT interval prolongation

            Hyperglycemia

            Hyperkalemia

            Hypomagnesemia

            Neutropenia

            Pancytopenia

            <1%

            Peripheral arterial occlusive disease

            Tumor lysis syndrome

            Aortic valve sclerosis

            Abscess

            Amnesia

            Dehydration

            Postmarketing Reports

            Infections: Hepatitis B virus reactivation

            Sepsis, subcutaneous abscess, anal abscess, furuncle, tinea pedis

            Thrombotic microangiopathy

            Nervous system disorders: Facial paralysis

            Previous
            Next:

            Warnings

            Black Box Warnings

            QT prolongation

            • Prolongs QT interval; sudden death reported
            • Do not use in patients with hypokalemia, hypomagnesemia, or long QT syndrome
            • Must correct hypokalemia or hypomagnesemia before initiating therapy
            • Monitor potassium and magnesium periodically
            • Avoid drugs known to prolong QT and strong CYP3A4 inhibitors
            • Reduced dose with hepatic impairment
            • Monitor QTc through electrocardiograms (ECGs) at baseline, 7 days after initiation, and periodically thereafter following any dose adjustments
            • Take on empty stomach; avoid food 2 hr before and 1 hr after taking dose

            Contraindications

            Long QT syndrome, hypokalemia, hypomagnesemia

            Cautions

            Grade 3/4 thrombocytopenia, neutropenia and anemia may occur (see Dosage Modifications); perform CBCs every 2 weeks for first 2 months and then monthly thereafter, or as clinically indicated; myelosuppression was generally reversible and usually managed by withholding drug temporarily or dose reduction

            Sudden deaths reported 0.3% of patients with CML treated with nilotinib; ventricular repolarization abnormalities may have contributed to their occurrence; evaluate cardiovascular status and monitor/manage cardiovascular risk factors during therapy

            Prolongs QT interval; significant prolongation of the QT interval may occur when drug is inappropriately taken with food; avoid taking with food; correct hypokalemia or hypomagnesemia before administration (see Black Box Warnings); prolongation of the QT interval can result in a type of ventricular tachycardia called Torsade de Pointes, which may result in syncope, seizure, and/or death

            Nilotinib can cause hypophosphatemia, hypokalemia, hyperkalemia, hypocalcemia, and hyponatremia; correct hypokalemia or hypomagnesemia before administration; monitor periodically during therapy

            Cardiovascular events (eg, ischemic heart disease, peripheral arterial occlusive disease and ischemic cerebrovascular events) reported in patients with newly diagnosed Ph+ CML; cardiovascular status should be evaluated and cardiovascular risk factors monitored and managed during therapy

            Use caution in history of pancreatitis; monitor serum lipase monthly or as clinically indicated; in case lipase elevations are accompanied by abdominal symptoms, interrupt doses and consider appropriate diagnostics to exclude pancreatitis

            Use caution in hepatic impairment; monitor hepatic function tests monthly or as clinically indicated; reduce dose and monitor QT interval

            May result in elevations in bilirubin, AST/ALT, and alkaline phosphatase; Grade 3-4 elevations of bilirubin, AST, and ALT were reported at higher frequency in pediatric than in adult patients; monitor hepatic function tests monthly or as clinically indicated

            Tumor lysis syndrome cases reported in nilotinib treated patients with resistant or intolerant CML; maintain adequate hydration and correct uric acid levels prior to initiating therapy

            Total gastrectomy may reduce nilotinib systemic exposure; perform more frequent follow-up of these patients; if necessary, consider dose increase or alternative therapy

            Hemorrhage from any site may occur; advise patients to report signs and symptoms of bleeding and medically manage as needed

            Monitor patients for signs of severe fluid retention (eg, unexpected rapid weight gain or swelling) and for symptoms of respiratory or cardiac compromise (eg, shortness of breath) during treatment; evaluate etiology and treat patients accordingly

            Women should be advised not to become pregnant while on therapy; may cause fetal harm (see Pregnancy)

            Growth retardation has been reported in pediatric patients with Ph+ CML in chronic phase receiving nilotinib

            Monitoring BCR-ABL transcript levels

            • Monitoring transcript levels in patients who discontinued therapy
              • Monitor BCR-ABL transcript levels in patients eligible for treatment discontinuation using an FDA authorized test validated to measure molecular response levels with a sensitivity of at least MR4.5 (BCR-ABL/ABL ≤ 0.0032% IS)
              • In patients who discontinue therapy, assess BCR-ABL transcript levels monthly for one year, then every 6 weeks for the second year and every 12 weeks thereafter during treatment discontinuation
              • Newly diagnosed patients must reinitiate therapy within 4 weeks of a loss of major molecular response [(MMR), corresponding to MR3.0 or = BCR-ABL/ABL ≤ 0.1% IS]
              • Patients resistant or intolerant to prior treatment which included imatinib must reinitiate therapy within 4 weeks of a loss of MMR or confirmed loss of MR4.0 (two consecutive measures separated by at least 4 weeks showing loss of MR4.0, corresponding to = BCR-ABL/ABL ≤ 0.01% IS)
              • For patients who fail to achieve MMR after three months of treatment reinitiation, BCR-ABL kinase domain mutation testing should be performed
            • Monitoring of BCR-ABL transcript levels in patients who have reinitiated therapy after loss of molecular response
              • Monitor CBC and BCR-ABL transcripts in patients who reinitiate treatment with Tasigna due to loss of molecular response quantitation every 4 weeks until a major molecular response is re-established, then every 12 weeks

            Drug interaction overview

            • Food increases blood levels of nilotinib; avoid food 2 hr before and 1 hour after a dose
            • Coadministration with a strong CYP3A inhibitor increased nilotinib concentrations and toxicities
            • Coadministration with a strong CYP3A inducer decreased nilotinib concentrations and toxicities
            • Should treatment with any HMG-CoA reductase inhibitor (a lipid lowering agent) be needed to treat lipid elevations, evaluate potential for a drug-drug interaction before initiation
            • Contains lactose; avoid in galactose intolerance, lactase deficiency or glucose-galactose malabsorption
            • Drugs that affect gastric pH
              • Nilotinib has pH-dependent solubility, with decreased solubility at higher pH that may reduce its bioavailability
              • Coadministration with PPIs not recommended; PPIs decrease nilotinib AUC by ~34%
              • Administer H2 blockers ~10 hr before or 2 hr after nilotinib dose
              • Administer antacids 2 hr before or after nilotinib dose
            • Effects of nilotinib on drug metabolizing enzymes and drug transport systems
              • Nilotinib is a competitive inhibitor of CYP3A4, CYP2C8, CYP2C9, CYP2D6 and UGT1A1 in vitro, potentially increasing the concentrations of drugs eliminated by these enzymes
              • Nilotinib may induce CYP2B6, CYP2C8 and CYP2C9, and decrease the concentrations of drugs which are eliminated by these enzymes
              • Nilotinib inhibits human P-glycoprotein (P-gp); drugs that inhibit P-gp, increased concentrations of nilotinib are likely, and caution should be exercised
            Previous
            Next:

            Pregnancy & Lactation

            Pregnancy

            No available data in pregnant women to inform the drug-associated risk; in animal reproduction studies, administration of nilotinib to pregnant rats and rabbits during organogenesis caused adverse developmental outcomes including embryo-fetal lethality, fetal effects, and fetal variations in rats and rabbits at maternal exposures (AUC) approximately 2 and 0.5 times, respectively, exposures in patients at recommended dose; advise pregnant women of potential risk to fetus

            Pregnancy test

            • Females of reproductive potential should have a pregnancy test prior to starting treatment

            Contraception

            • Based on animal studies, drug can cause fetal harm when administered to a pregnant woman; advise females of reproductive potential to use effective contraception during treatment with drug and for at least 14 days after the last dose

            Infertility

            • The risk of infertility in females or males of reproductive potential has not been studied in humans; in studies in rats and rabbits, the fertility in males and females was not affected

            Lactation

            No data are available regarding the presence of nilotinib or its metabolites in human milk or its effects on a breastfed child or on milk production

            However, nilotinib is present in the milk of lactating rats

            Owing to the potential for serious adverse reactions in a nursing child, advise lactating women not to breastfeed during treatment and for at least 14 days after the last dose

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

            Previous
            Next:

            Pharmacology

            Mechanism of Action

            Selectively binds with high affinity to ATP-binding site of BCR-ABL kinase inhibiting cell proliferation in cell lines and in primary Ph+ CML leukemia cells

            Active against imatinib-resistant mutant forms of Bcr-Abl

            Inhibits PDGFR and c-Kit kinase

            Absorption

            Peak plasma concentration: 1,540 ng/ml (300 mg BID)

            AUC: 13,337 ng·hr/ml (300 mg BID)

            Peak plasma time: 3 hr

            Distribution

            Protein Bound: 98%

            Blood-to-serum ratio: 0.68

            Metabolism

            Oxidation and hydroxylation by liver CYP3A4

            Enzymes Inhibited: CYP3A4, CYP2C8, CYP2C9, CYP2D6, UGT1A1

            Enzymes Induced CYP2B6, CYP2C8, CYP2C9

            Elimination

            Half-life: ~17 hr

            Clearance: ~29 L/hr

            Excretion: Feces 93%

            Pharmacogenomics

            Confirmed BCR-ABL transcripts

            • Tyrosine kinase inhibitors (TKIs) inhibit activity of BCR-ABL fusion protein, resulting in both hematologic response (ie, normal cell counts in the peripheral blood and normal bone marrow morphology), as well as cytogenetic response (ie, disappearance or reduction of the Philadelphia [Ph] chromosome)
            • NCCN clinical practice guidelines recommends TKIs in CML with confirmed BCR-ABL transcripts in bone marrow or evidence of translocation on cytogenetics

            UGT1A1 and increased bilirubin

            • Polymorphisms of UGT1A1 and its potential association with hyperbilirubinemia during nilotinib treatment have been studied
            • The (TA)7/(TA)7 genotype was associated with a statistically significant increase in the risk of hyperbilirubinemia relative to the (TA)6/(TA)6 and (TA)6/(TA)7 genotypes
            • However, the largest increases in bilirubin were observed in the (TA)7/(TA)7 genotype (UGT1A1*28) patients during nilotinib treatment

            Genetic testing laboratories

            • The following companies currently offer FISH and/or transcript quantification testing for BCR-ABL
            • Asuragen (http://www.asuragen.com/)
            • Dako (http://www.dakousa.com/)
            • Invitrogen (http://www.invitrogen.com/)
            • Ipsogen (http://www.ipsogen.com)
            Previous
            Next:

            Administration

            Oral Administration

            Take twice daily at ~12-hr intervals (unless dosage modification required)

            Administer on empty stomach; do not consume food for at least 2 before the dose and for at least 1 hr after the dose is taken

            Swallow capsule whole with water

            If unable to swallow capsules, capsule contents may be dispersed in 1 teaspoon of applesauce; take mixture immediately (within 15 minutes) and do not be stored for future use

            Missed dose

            • If a dose is missed, take the next dose as scheduled
            • Do not double dose to make up for missed doses

            Storage

            Tablets: Store at room temperature between 68-77°F (20-25°C)

            Previous
            Next:

            Images

            BRAND FORM. UNIT PRICE PILL IMAGE
            Tasigna oral
            -
            200 mg capsule

            Copyright © 2010 First DataBank, Inc.

            Previous
            Next:

            Patient Handout

            Patient Education
            nilotinib oral

            NILOTINIB - ORAL

            (nye-LOE-ti-nib)

            COMMON BRAND NAME(S): Tasigna

            WARNING: This drug can rarely cause serious (possibly fatal) irregular heartbeats (QT prolongation). Nilotinib should not be used in people with low blood levels of certain minerals (potassium, magnesium) or a certain heart problem (long QT syndrome). To lower your risk, your doctor will order certain blood tests (potassium/magnesium levels, liver function tests) before and during treatment with nilotinib. You should have a heart test (EKG) before starting nilotinib. The EKG should be repeated 7 days after your first dose, when your dose is changed, and periodically while you are taking nilotinib.To decrease the risk of this effect, do not eat for 2 hours before or 1 hour after taking your dose. Other drugs/foods may increase the risk of an irregular heartbeat. Before taking this drug, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. See also How to Use and Drug Interactions sections.

            USES: Nilotinib is used to treat a certain type of blood cancer (chronic myelogenous leukemia-CML). It works by slowing or stopping the growth of cancer cells.

            HOW TO USE: Read the Medication Guide provided by your pharmacist before you start using nilotinib and each time you get a refill. If you have any questions, consult your doctor or pharmacist.Avoid eating grapefruit or drinking grapefruit juice while being treated with this medication unless your doctor instructs you otherwise. Grapefruit can increase the amount of certain medications in your bloodstream. Consult your doctor or pharmacist for more details.Take this medication by mouth on an empty stomach, usually twice daily about 12 hours apart or as directed by your doctor. Swallow the capsule whole with water. Do not open, break, or chew the capsules. Do not eat any food for at least 2 hours before or for 1 hour after taking your dose. Taking this medication with food can increase the amount of drug in your body and increase the risk of serious side effects. If unable to swallow the capsules, the capsules may be opened and the contents sprinkled in 1 teaspoon of applesauce. This mixture should be swallowed right away (within 15 minutes). Use only 1 teaspoon of applesauce. Do not sprinkle the contents onto other types of food.Drink plenty of fluids during treatment with this medication, unless otherwise directed by your doctor.If you are also taking an antacid, take it 2 hours before or after nilotinib. If you are also taking an H2 blocker (such as cimetidine, famotidine), take it 10 hours before or 2 hours after nilotinib.The dosage is based on your medical condition, response to treatment, laboratory tests, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products). Children's dosage is also based on body size.Do not increase your dose or take this medication more often than prescribed. Your condition will not improve any faster, and the risk of serious side effects may be increased.Since this drug can be absorbed through the skin and lungs, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the contents of the capsules.

            SIDE EFFECTS: See also Warning section.Nausea, vomiting, headache, tiredness, constipation, and diarrhea may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.People using this medication may have serious side effects. However, you have been prescribed this drug because your doctor has judged that the benefit to you is greater than the risk of side effects. Careful monitoring by your doctor may decrease your risk.This medication decreases bone marrow function, an effect that may lead to a low number of blood cells such as red cells, white cells, and platelets. This effect can cause anemia, decrease your body's ability to fight an infection, or cause easy bruising/bleeding. Tell your doctor right away if you develop any of the following serious symptoms: severe tiredness, pale skin, signs of infection (such as fever, chills, persistent sore throat), easy bruising/bleeding (such as bloody/black stool, bloody/pink urine).Nilotinib sometimes causes side effects due to the rapid destruction of cancer cells (tumor lysis syndrome). To lower your risk, your doctor may add a medication and tell you to drink plenty of fluids. Tell your doctor right away if you have symptoms such as: low back/side pain (flank pain), signs of kidney problems (such as painful urination, change in the amount of urine), muscle spasms/weakness.Tell your doctor right away if you have any serious side effects, including: severe stomach/abdominal pain, toe/joint pain, swelling hands/ankles/feet, unusual/rapid weight gain, symptoms of high blood sugar (such as increased thirst/urination), signs of liver disease (such as persistent nausea/vomiting, stomach/abdominal pain, yellowing eyes/skin, dark urine).Get medical help right away if you have any very serious side effects, including: fast/pounding/irregular heartbeat, severe dizziness, fainting, seizures, signs of a heart attack (such as chest/jaw/left arm pain, shortness of breath, unusual sweating), signs of a stroke (such as weakness on one side of the body, trouble speaking, sudden vision changes, confusion), signs of bleeding in the brain (such as sudden severe headache, sudden vision changes, confusion, loss of consciousness), signs of blood circulation disease (such as numbness/pain in the legs, leg pain with physical activity, decrease in walking distance).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

            PRECAUTIONS: Before taking nilotinib, tell your doctor or pharmacist if you are allergic to it; or to lactose/galactose; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, pancreatitis, heart disease (such as coronary artery disease, chest pain, heart attack), high blood pressure, high cholesterol, diabetes, stroke (including "mini-strokes" or transient ischemic attacks), blood circulation disease (peripheral arterial disease), blood vessel disease (hardening of the arteries/atherosclerosis), stomach surgery (such as gastrectomy).Nilotinib may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using nilotinib, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/"water pills") or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using nilotinib safely.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Nilotinib can make you more likely to get infections or may worsen any current infections. Wash your hands well to prevent the spread of infection. Avoid contact with people who have infections that may spread to others (such as chickenpox, measles, flu). Consult your doctor if you have been exposed to an infection or for more details.Do not have immunizations/vaccinations without the consent of your doctor. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).To lower the chance of getting cut, bruised, or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports.Children may be more sensitive to the side effects of this drug, especially liver disease, and slowed growth and development. Consult the doctor or pharmacist for more details. See the doctor regularly so your child's liver function, height, weight, and development can be checked.Older adults may be more sensitive to the side effects of this drug, especially QT prolongation (see above).Tell your doctor if you are pregnant or plan to become pregnant. You should not become pregnant while using nilotinib. Nilotinib may harm an unborn baby. Ask about reliable forms of birth control while using this medication and for 14 days after stopping treatment. If you become pregnant, talk to your doctor right away about the risks and benefits of this medication.It is not known whether this drug passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this drug and for 14 days after stopping treatment is not recommended. Consult your doctor before breast-feeding.

            DRUG INTERACTIONS: See also How to Use.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: antacids, flibanserin, H2 blockers (such as cimetidine/famotidine), proton pump inhibitors (such as omeprazole).Other medications can affect the removal of nilotinib from your body, which may affect how nilotinib works. Examples include azole antifungals (such as itraconazole, ketoconazole), HIV protease inhibitors (such as ritonavir), macrolide antibiotics (such as clarithromycin), rifamycins (such as rifabutin), St. John's wort, drugs used to treat seizures (such as carbamazepine, phenytoin), among others.Many drugs besides nilotinib may affect the heart rhythm (QT prolongation), including amiodarone, dofetilide, pimozide, procainamide, quinidine, sotalol, macrolide antibiotics (such as erythromycin), among others.

            OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

            NOTES: Do not share this medication with others.Lab and/or medical tests (such as growth and development checks for children, complete blood count, EKG, electrolyte levels, liver function, lipase levels, uric acid level, cholesterol and blood sugar levels) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

            MISSED DOSE: If you miss a dose, take it as soon as you remember, but do not take if it is less than 2 hours before or 1 hour after a meal. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

            STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

            MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).

            Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

            IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

            Previous
            Next:

            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
            Additional Offers
            Email to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Email Forms to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Previous
            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.